Montgomery Stuart A
Imperial College School of Medicine, University of London, London, United Kingdom.
CNS Spectr. 2008 Jul;13(7 Suppl 11):27-33. doi: 10.1017/s1092852900028297.
All three serotonin norepinephrine reuptake inhibitors (SNRIs) inhibit the reuptake of both serotonin and norepinephrine but they do so with differing affinity ratios. Venlafaxine has a 30-fold higher affinity for serotonin than for norepinephrine while duloxetine has a 10-fold selectivity for serotonin. Milnacipran has a balanced (1:1) ratio of potency for inhibition of reuptake of the two neurotransmitters. The most frequent adverse event with SNRIs is nausea. Not unexpectedly, adverse effects related to a noradrenergic stimulation, such as dry mouth, sweating, and constipation, are found more frequently with SNRIs than with selective serotonin reuptake inhibitors. At true SNRI doses, venlafaxine is associated with dose-dependent cardiovascular phenomena (principally increased blood pressure), an effect which is less frequent with duloxetine and rare with milnacipran. Serious and potentially fatal hepatotoxity has been reported with duloxetine. This problem appears to be unique to duloxetine and not a characteristic of the SNRI class. There are differences in overdose toxicity between venlafaxine and the other SNRIs, possibly related to its increased cardiotoxicity.
所有三种5-羟色胺去甲肾上腺素再摄取抑制剂（SNRIs）均能抑制5-羟色胺和去甲肾上腺素的再摄取，但它们的亲和力比值不同。文拉法辛对5-羟色胺的亲和力比对去甲肾上腺素高30倍，而度洛西汀对5-羟色胺具有10倍的选择性。米那普明对两种神经递质再摄取抑制的效价具有平衡的（1:1）比值。SNRIs最常见的不良事件是恶心。不出所料，与去甲肾上腺素能刺激相关的不良反应，如口干、出汗和便秘，在使用SNRIs时比使用选择性5-羟色胺再摄取抑制剂时更常见。在真正的SNRI剂量下，文拉法辛与剂量依赖性心血管现象（主要是血压升高）有关，度洛西汀出现这种效应的频率较低，米那普明则很少见。度洛西汀已报告有严重且可能致命的肝毒性。这个问题似乎是度洛西汀独有的，并非SNRI类药物的特征。文拉法辛与其他SNRIs在过量毒性方面存在差异，这可能与其增加的心脏毒性有关。
